计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
BIX 02188是一种选择性的MEK5抑制剂，IC50为4.3 nM，也抑制ERK5催化活性，IC50为810 nM，且不抑制与其密切相关的激酶MEK1， MEK2， ERK2，和JNK2
Information
BIX02188 is a selective inhibitor ofMEK5withIC50of 4.3 nM, also inhibits ERK5 catalytic activity withIC50of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
In vitro
BIX02188 significantly blocks MEK5 catalytic activity with IC50 of 4.3 nM and inhibits ERK5 catalytic activity with IC50 of 0.83 μM. It shows no activity against closely related kinases MEK1, MEK2, ERK1, p38α, JNK2, TGFβR1, EGFR, and STK16 with IC50 values of 1.8 μM for TGFβR1, 3.9 μM for p38α, and >6.3 μM for other kinases. Pretreatment with BIX02188 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. BIX02188 treatment alone for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02188 inhibits transcriptional activation of MEF2C through the MEK5/ERK5 signaling cascade in active MEK5/ERK5/MEF2C-driven luciferase expression system in HeLa and HEK293 cells with IC50 values of 1.15 μM and 0.82 μM, respectively. BIX02188 also inhibits phosphorylation of BMK1 in bovine lung microvascular endothelial cells (BLMECs) which are stimulated with 300 μM H2O2, in a dose-dependent manner, with IC50 of 0.8 μM, specifically by blocking the MEK5 signal pathway. BIX02188 completely reverses the inhibitory effect on TNF-mediation; JNK activation had a similar effect on BMK1 inhibition, suggesting that it inhibits TNF signaling through activation of the MEK5-BMK1 signaling pathway.
In vivo
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentration ~10 μM
Incubation Time：Pretreatment for 1.5 hours
Powder Purity:≥99%
规格
英文别名
(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
BIX 02188
生化机理
BIX02188 是 MEK5 的选择性抑制剂，IC50 为 4.3 nM，也能抑制 ERK5 的催化活性，IC50 为 810 nM，但不抑制密切相关的激酶 MEK1、MEK2、ERK2 和 JNK2。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
丝裂原活化蛋白激酶 7 抑制剂;丝裂原活化蛋白激酶 5 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N)O
分子量
412.48
Reaxy-Rn
60405314
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=60405314&ln=
技术文档
高级数据
关联靶点（人）
MAPK7
Tchem
丝裂原活化蛋白激酶 7(Mitogen-activated protein kinase 7)
(1 活性数据)
MAP2K5
Tchem
双特异性丝裂原活化蛋白激酶激酶 5(Dual specificity mitogen-activated protein kinase kinase 5)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 49 mg/mL (200.62 mM); Ethanol: 49 mg/mL (200.62 mM); Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
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